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Discovery of 9‑Cyclopropylethynyl-2-((S)‑1-[1,4]dioxan-2-ylmethoxy)-6,7-dihydropyrimido[6,1‑a]-isoquinolin-4-one (GLPG1205), a Unique GPR84 Negative Allosteric Modulator Undergoing Evaluation in a Phase II Clinical Trial.

Autor: Labéguère, Frédéric, Dupont, Sonia, Alvey, Luke, Soulas, Florilène, Newsome, Gregory, Tirera, Amynata, Quenehen, Vanessa, Mai, Thi Thu Trang, Deprez, Pierre, Blanqué, Roland, Oste, Line, Le Tallec, Sandrine, De Vos, Steve, Hagers, Annick, Vandevelde, Ann, Nelles, Luc, Vandervoort, Nele, Conrath, Katja, Christophe, Thierry, van der Aar, Ellen

Publikováno v: Journal of Medicinal Chemistry; 12/10/2020, Vol. 63 Issue 23, p13526-13545, 20p

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Synthesis of the Novel Amino Acid 4-Amino-3-(aminomethyl)benzoic Acid (AmAbz) and Its Protected Derivatives as Building Blocks for Pseudopeptide Synthesis

Autor: Pascal, Robert, Sola, Régine, Labéguère, Frédéric, Jouin, Patrick

Publikováno v: European Journal of Organic Chemistry; November 2000, Vol. 2000 Issue: 22 p3755-3761, 7p

Three classes of ligands each bind to distinct sites on the orphan G protein-coupled receptor GPR84.

Autor: Mahmud ZA; Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow Glasgow, G12 8QQ, Scotland, United Kingdom., Jenkins L; Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow Glasgow, G12 8QQ, Scotland, United Kingdom., Ulven T; Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, DK-5230, Odense M, Denmark., Labéguère F; Galapagos SASU, 102 Avenue Gaston Roussel, 93230, Romainville, France.; Evotec, 195 Route d'Espagne, 31100, Toulouse, France., Gosmini R; Galapagos SASU, 102 Avenue Gaston Roussel, 93230, Romainville, France., De Vos S; Galapagos NV, Generaal De Wittelaan L11 A3, 2800, Mechelen, Belgium., Hudson BD; Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow Glasgow, G12 8QQ, Scotland, United Kingdom., Tikhonova IG; School of Pharmacy, Medical Biology Centre, Queen's University Belfast, Belfast, BT9 7BL, United Kingdom., Milligan G; Centre for Translational Pharmacology, Institute of Molecular, Cell and Systems Biology, College of Medical, Veterinary and Life Sciences, University of Glasgow Glasgow, G12 8QQ, Scotland, United Kingdom. Graeme.Milligan@glasgow.ac.uk.

Publikováno v: Scientific reports [Sci Rep] 2017 Dec 20; Vol. 7 (1), pp. 17953. Date of Electronic Publication: 2017 Dec 20.